Bioorganic and Medicinal Chemistry Letters p. 2013 - 2018 (1999)
Update date:2022-09-26
Topics:
Buijsman, Rogier C.
Basten, Jan E. M.
Van Dinther, Theo G.
Van der Marel, Gijsbert A.
Van Boeckel, Constant A. A.
Van Boom, Jacques H.
The synthesis of a novel antithrombotic consisting of a heparin pentasaccharide conjugated to the active site inhibitor N-(2- naphtalenesulfonyl)-glycyl-(D)-4-aminophenyl-alanyl-piperidine (NAPAP) (i.e. compound I) is reported. This conjugate shows a unique pharmacological profile both in vitro and in vivo having direct anti-thrombin and ATIII- mediated anti-Xa activity. Furthermore, conjugate I has a prolonged in vivo half-life compared to NAPAP (1.5 h vs 9 min.).
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